carboxamide ] , a New Potent and Selective Antagonist of the CB 1 Cannabinoid Receptor : Biochemical and Pharmacological Characterization

@inproceedings{RinaldiCarmona2004carboxamide,
  title={carboxamide ] , a New Potent and Selective Antagonist of the CB 1 Cannabinoid Receptor : Biochemical and Pharmacological Characterization},
  author={Murielle Rinaldi-Carmona and Francis X Barth and Christian Congy and Serge A. Martinez and Didier Oustric and Alain P{\'e}rio and Martine Poncelet and Jeanne Maruani and Mich{\`e}le Arnone and Olivier Finance and Philippe Soubri{\'e} and G{\'e}rard le Fur},
  year={2004}
}
Based on binding, functional, and pharmacological data, this study introduces SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide] as a highly potent, selective, and orally active antagonist for the CB1 receptor. This compound displays nanomolar affinity (Ki 0.56 and 3.5 nM) for both the rat brain and human CB1 recombinant receptors, respectively. It has low affinity (Ki 400 nM) for both the rat spleen and human CB2 receptors. Furthermore, it… CONTINUE READING
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